Prevalence of Masked Obesity Associated with Lifestyle-Related Habits, Dietary Habits, and Energy Metabolism in Japanese Young Women

We investigated the prevalence of Masked Obesity (MO) and the correlations between MO and lifestylerelated habits (e.g., exercise habits, dieting habits), dietary habits, energy metabolism, and seasons. The subjects were 131 young Japanese college students. Body composition was measured by bioelectrical impedance method and Resting Metabolic Rate (RMR) was measured by an indirect calorimeter. Subjects with a BMI in the normal range (n=110) were divided into the MO (percentage of body fat to Body Weight [BF]≥30%) and control (C) (BF<30%) groups. Dietary energy and nutrient intakes were calculated from weighed dietary records. A questionnaire on lifestyle habits was obtained individually from the subjects. The percentage of MO was 32% of subjects within normal BMI. The prevalence of MO was the highest in winter, probably due to accumulation of body fat as an adaptation to cold. The MO group had low Fat-Free Mass (FFM) and high BF. RMR of the MO group was significantly lower than that of the C group. The MO group tended to have poor exercise habits, more dieting (restricting calorie intake) experiences and consumed a diet with less vegetables and beans. We concluded that the prevalence of MO was 32%; it was the highest in winter for subjects who had high fat and low FFM. This fact may be due to poor exercise, more dieting experiences and insufficient intake of vegetables and beans. Furthermore, this accumulation of body fat may be partly due to low RMR

Relationship between Seasonal Changes in Food Intake and Energy Metabolism, Physical Activity, and Body Composition in Young Japanese Women

We investigated seasonal changes in food intake, energy metabolism, and physical activity (PA) and explored their associations with body composition. In total, 28 women aged 20–23 years in the Kansai area of Japan participated in this year-long study spanning the winter, spring, and summer seasons. A dietary investigation was performed using the weight recording method, and the amount of histidine in the diet, which may be related to the regulation of energy intake, was calculated. Resting metabolic rate (RMR), body composition, and PA were measured using indirect calorimetry, bioelectrical impedance analysis, and uniaxial accelerometry, respectively. The results showed that energy intake was highest in winter, decreased significantly with increasing temperature, and decreased by 25% in summer. As the intake of histidine in the diet did not increase in summer, it did not seem to be involved in the suppression of energy intake. RMR was highest in winter and decreased significantly in summer by 20%. The amount of PA was low in winter, increased significantly in the spring, and decreased again in summer. Body weight increased in winter, with an accumulation of fat in the trunk and arms, and decreased in summer, with a reduction in the amount of fat. Greater energy intake and less PA in winter induced an increment in body weight despite the increase in RMR. There were no significant changes in lean body mass between the seasons; however, the muscle weight of the lower limbs increased significantly in spring and in summer compared with that in winter (p < 0.001). Thus, seasonal changes in food intake, energy metabolism, and PA occur, with resultant changes in the body composition under comfortable air-conditioned environments

Cross-Stacked Single-Crystal Organic Nanowire p–n Nanojunction Arrays by Nanotransfer Printing

We fabricated cross-stacked organic p–n nanojunction arrays made of single-crystal 6,13-bis­(triisopropylsilylethynyl) pentacene (TIPS-PEN) and fullerene (C₆₀) nanowires as p-type and n-type semiconductors, respectively, by using a nanotransfer printing technique. Single-crystal C₆₀ nanowires were synthesized inside nanoscale channels of a mold and directly transferred onto a desired position of a flexible substrate by a lubricant liquid layer. In the consecutive printing process, single-crystal TIPS-PEN nanowires were grown in the same way and then perpendicularly aligned and placed onto the C₆₀ nanowire arrays, resulting in a cross-stacked single-crystal organic p–n nanojunction array. The cross-stacked single-crystal TIPS-PEN/C₆₀ nanowire p–n nanojunction devices show rectifying behavior with on/off ratio of ∼13 as well as photodiode characteristic with photogain of ∼2 under a light intensity of 12.2 mW/cm². Our study provides a facile, solution-processed approach to fabricate a large-area array of organic crystal nanojunction devices in a desired arrangement for future nanoscale electronics

Crystal Structures of Tetramorphic Forms of Donepezil and Energy/Temperature Phase Diagram via Direct Heat Capacity Measurements

Donepezil is used for the palliative treatment of mild to moderate dementia of the Alzheimer’s disease. Donepezil crystallized as four solvent-free polymorphs including forms I, II, C, and F which differ in molecular conformations and packing. Conformational difference comes from the torsion of the 2, 3-dihydroinden-1-one moiety and methyl-benzyl ring with respect to piperidyl ring. Similar melting temperatures and heats of fusion were observed for four solvent-free polymorphic forms and made polymorph selection by solvent crystallization method poor. The relative thermodynamic stability relationships of each polymorph with respect to the amorphous form were determined using direct heat capacity (<i>C</i>_<i>p</i>) measurement and then used to evaluate the relative thermodynamic stability between polymorphs. Form F was the stable form over the temperature ranges we studied. Other than form F, form C was the stable form among three polymorphic forms including I, II, and C, below 53 °C, and is enantiotropically related to both forms I and II. Form II is the stable form above 53 °C and monotropically related to form I. The thermodynamic relationships between polymorphs were further confirmed by measuring the solubility over temperatures ranging from 35 to 60 °C in ethanol. Slurry conversion in ethanol, isopropyl alcohol, and cyclohexane was conducted to provide a guideline to obtain pure and desired polymorphic forms. The establishment of the thermodynamic relationships among four polymorphic forms greatly facilitated polymorph selections of donepezil

Crystal Structures of Tetramorphic Forms of Donepezil and Energy/Temperature Phase Diagram via Direct Heat Capacity Measurements

Donepezil is used for the palliative treatment of mild to moderate dementia of the Alzheimer’s disease. Donepezil crystallized as four solvent-free polymorphs including forms I, II, C, and F which differ in molecular conformations and packing. Conformational difference comes from the torsion of the 2, 3-dihydroinden-1-one moiety and methyl-benzyl ring with respect to piperidyl ring. Similar melting temperatures and heats of fusion were observed for four solvent-free polymorphic forms and made polymorph selection by solvent crystallization method poor. The relative thermodynamic stability relationships of each polymorph with respect to the amorphous form were determined using direct heat capacity (<i>C</i>_<i>p</i>) measurement and then used to evaluate the relative thermodynamic stability between polymorphs. Form F was the stable form over the temperature ranges we studied. Other than form F, form C was the stable form among three polymorphic forms including I, II, and C, below 53 °C, and is enantiotropically related to both forms I and II. Form II is the stable form above 53 °C and monotropically related to form I. The thermodynamic relationships between polymorphs were further confirmed by measuring the solubility over temperatures ranging from 35 to 60 °C in ethanol. Slurry conversion in ethanol, isopropyl alcohol, and cyclohexane was conducted to provide a guideline to obtain pure and desired polymorphic forms. The establishment of the thermodynamic relationships among four polymorphic forms greatly facilitated polymorph selections of donepezil

Crystal Structures of Tetramorphic Forms of Donepezil and Energy/Temperature Phase Diagram via Direct Heat Capacity Measurements

Donepezil is used for the palliative treatment of mild to moderate dementia of the Alzheimer’s disease. Donepezil crystallized as four solvent-free polymorphs including forms I, II, C, and F which differ in molecular conformations and packing. Conformational difference comes from the torsion of the 2, 3-dihydroinden-1-one moiety and methyl-benzyl ring with respect to piperidyl ring. Similar melting temperatures and heats of fusion were observed for four solvent-free polymorphic forms and made polymorph selection by solvent crystallization method poor. The relative thermodynamic stability relationships of each polymorph with respect to the amorphous form were determined using direct heat capacity (<i>C</i>_<i>p</i>) measurement and then used to evaluate the relative thermodynamic stability between polymorphs. Form F was the stable form over the temperature ranges we studied. Other than form F, form C was the stable form among three polymorphic forms including I, II, and C, below 53 °C, and is enantiotropically related to both forms I and II. Form II is the stable form above 53 °C and monotropically related to form I. The thermodynamic relationships between polymorphs were further confirmed by measuring the solubility over temperatures ranging from 35 to 60 °C in ethanol. Slurry conversion in ethanol, isopropyl alcohol, and cyclohexane was conducted to provide a guideline to obtain pure and desired polymorphic forms. The establishment of the thermodynamic relationships among four polymorphic forms greatly facilitated polymorph selections of donepezil

Crystal Structures of Tetramorphic Forms of Donepezil and Energy/Temperature Phase Diagram via Direct Heat Capacity Measurements

Donepezil is used for the palliative treatment of mild to moderate dementia of the Alzheimer’s disease. Donepezil crystallized as four solvent-free polymorphs including forms I, II, C, and F which differ in molecular conformations and packing. Conformational difference comes from the torsion of the 2, 3-dihydroinden-1-one moiety and methyl-benzyl ring with respect to piperidyl ring. Similar melting temperatures and heats of fusion were observed for four solvent-free polymorphic forms and made polymorph selection by solvent crystallization method poor. The relative thermodynamic stability relationships of each polymorph with respect to the amorphous form were determined using direct heat capacity (<i>C</i>_<i>p</i>) measurement and then used to evaluate the relative thermodynamic stability between polymorphs. Form F was the stable form over the temperature ranges we studied. Other than form F, form C was the stable form among three polymorphic forms including I, II, and C, below 53 °C, and is enantiotropically related to both forms I and II. Form II is the stable form above 53 °C and monotropically related to form I. The thermodynamic relationships between polymorphs were further confirmed by measuring the solubility over temperatures ranging from 35 to 60 °C in ethanol. Slurry conversion in ethanol, isopropyl alcohol, and cyclohexane was conducted to provide a guideline to obtain pure and desired polymorphic forms. The establishment of the thermodynamic relationships among four polymorphic forms greatly facilitated polymorph selections of donepezil

Crystal Structures of Tetramorphic Forms of Donepezil and Energy/Temperature Phase Diagram via Direct Heat Capacity Measurements

Donepezil is used for the palliative treatment of mild to moderate dementia of the Alzheimer’s disease. Donepezil crystallized as four solvent-free polymorphs including forms I, II, C, and F which differ in molecular conformations and packing. Conformational difference comes from the torsion of the 2, 3-dihydroinden-1-one moiety and methyl-benzyl ring with respect to piperidyl ring. Similar melting temperatures and heats of fusion were observed for four solvent-free polymorphic forms and made polymorph selection by solvent crystallization method poor. The relative thermodynamic stability relationships of each polymorph with respect to the amorphous form were determined using direct heat capacity (<i>C</i>_<i>p</i>) measurement and then used to evaluate the relative thermodynamic stability between polymorphs. Form F was the stable form over the temperature ranges we studied. Other than form F, form C was the stable form among three polymorphic forms including I, II, and C, below 53 °C, and is enantiotropically related to both forms I and II. Form II is the stable form above 53 °C and monotropically related to form I. The thermodynamic relationships between polymorphs were further confirmed by measuring the solubility over temperatures ranging from 35 to 60 °C in ethanol. Slurry conversion in ethanol, isopropyl alcohol, and cyclohexane was conducted to provide a guideline to obtain pure and desired polymorphic forms. The establishment of the thermodynamic relationships among four polymorphic forms greatly facilitated polymorph selections of donepezil

Multicomponent System of NPS-1034, an Orally Administered Lung Cancer Drug Candidate, with Sulfonic Acids and Solid State Characterization

NPS-1034 is a drug candidate targeted for the regulation of c-MET/AXL receptor tyrosin kinase activity. NPS-1034 was developed to improve efficacy and reduce toxicity by targeting c-MET/AXL related signaling pathways. However, NPS-1034 is practically insoluble in almost all organic solvents as well as aqueous media (pH 1, 4.5, and 7.5). We attempted to improve the physicochemical properties of NPS-1034 by forming multicomponent systems with a wide variety of sulfonic acids including methanesulfonic acid, 1,2-ethanedisulfonic acid, <i>p</i>-toluenesulfonic acid, and camphorsulfonic acid. Solid state characterization of NPS-1034 salts and amorphous with sulfonic acids was conducted, and the crystal structures of four salts and NPS-1034 were compared and investigated. Sulfonic acid salts of NPS-1034 decreased the melting point of NPS-1034 as much as −155.43 °C. Solubilities of NPS-1034 and salts of NPS-1034 were measured to develop lipid-based formulation for the GLP toxicity study. Solvents studied include oleic acid, poly­(ethylene glycol) 400, and ethanol. Solubility of amorphous of NPS-1034 with camphorsulfonic acid showed a significant increase in all three solvents. This work will give some insight into how various types of sulfonic acids interact with pharmaceutically important compounds containing the pyrrolepyridine moiety